Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/232.5)
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Publication number: 20100160308Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 24, 2010Inventors: Jianping Cai, Shaoqing Chen, Yi Chen, Xin-Jie Chu, Robert Alan Goodnow, JR., Kang Le, Kin-Chun Luk, Steven Gregory Mischke, Peter Michael Wovkulich
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Publication number: 20100160255Abstract: The present invention provides a compound represented by the formula (I): wherein E is an optionally substituted cyclic group; D is a carbonyl group or a sulfonyl group; A is CH or N; ring P is an optionally further substituted 5- to 7-membered ring; ring Q is an optionally further substituted 5- to 7-membered nonaromatic ring; and ring R is an optionally further substituted and optionally condensed 5- to 7-membered nonaromatic ring, or a salt thereof. The compound of the present invention has an ACC inhibitory activity, is useful for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and has superior properties in the efficacy, duration of activity, specificity, low toxicity and the like.Type: ApplicationFiled: July 28, 2006Publication date: June 24, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Makoto Kamata, Kohji Fukatsu, Tohru Yamashita, Naoki Furuyama, Satoshi Endo
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Patent number: 7727985Abstract: This invention provides beta-carboline compounds of formula I: wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.Type: GrantFiled: April 9, 2004Date of Patent: June 1, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
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Patent number: 7718653Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic ring which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: GrantFiled: July 16, 2008Date of Patent: May 18, 2010Assignee: AstraZeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Publication number: 20100120722Abstract: This invention relates to pyrimidine compounds of formula (I), formula (I?), and formula (I?): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, R5, U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).Type: ApplicationFiled: January 15, 2010Publication date: May 13, 2010Applicant: Synta Pharmaceuticals Corp.Inventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Keizo Koya, Masazumi Nagai
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Publication number: 20100093713Abstract: This invention provides beta-carboline compounds of formula wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: Millennium Pharmaceuticals, Inc.Inventors: Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
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Patent number: 7696203Abstract: Compounds of formula I: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N; and (iii) CH, O, C; the dotted lines represent two double bonds in the appropriate locations; and where Z is selected from S, O, C(?O), CH2 and NH are disclosed for use in inhibiting DNA-PK.Type: GrantFiled: April 13, 2006Date of Patent: April 13, 2010Assignees: Kudos Pharmaceuticals Limited, Cancer Research Technology LimitedInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Keith Allan Menear, Marc Geoffrey Hummersone, Xiao-ling Cockcroft, Mark Frigerio, Roger John Griffin, Bernard Thomas Golding, Ian Robert Hardcastle, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Kappusamy Saravanan, Marine Desage-El Murr
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Publication number: 20100069380Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for screening and identifying compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase. In particular, provided herein are assays for the identification of compounds that inhibit or reduce the activity of a bacterial peptidyl tRNA hydrolase. The methods provided herein provide a simple, sensitive assay for high-throughput screening of libraries of compounds to identify pharmaceutical leads useful for preventing, treating, and managing a bacterial infection or one or more symptoms thereof. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: March 18, 2010Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Publication number: 20100069358Abstract: The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them.Type: ApplicationFiled: August 5, 2009Publication date: March 18, 2010Applicant: Eisai R&D Management Co., Ltd.Inventors: Piotr Pawel GRACZYK, Paschalis DIMOPOULOS, Christopher Neil FARTHING, Gurpreet Singh BHATIA, Afzal KHAN
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Patent number: 7678792Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit, PDGFR?, PDGFR?, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGF?, SRC, EGFR, trkB, FGFR3, FLT3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2?, BRK, KDR, c-raf or b-raf kinase, or mutant forms thereof.Type: GrantFiled: October 16, 2007Date of Patent: March 16, 2010Assignee: IRM LLCInventors: Donatella Chianelli, Christopher Cow, Yun He, Songchun Jiang, Xiaolin Li, Xiaodong Liu, Zuosheng Liu, Jon Loren, Valentina Molteni, Juliet Nabakka, Pingda Ren, Taebo Sim, Xiaodong Wang, Shuli You
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Publication number: 20100022529Abstract: The present invention provides amidophenoxyindazole compounds useful in the treatment of cancer.Type: ApplicationFiled: July 15, 2009Publication date: January 28, 2010Inventors: Tiechao LI, Mark Andrew POBANZ, Chuan SHIH, Zhipei WU, Wei Jennifer YANG, Boyu ZHONG
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Publication number: 20100009962Abstract: The present invention is directed to benzyl-substituted quinolone compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of diseases in which the M1 receptor is involved.Type: ApplicationFiled: June 27, 2007Publication date: January 14, 2010Inventors: Craig Lindsley, William D. Shipe, Feng Yang, Jaime Lynn Bunda
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Publication number: 20090318434Abstract: There is provided a process for the preparation of a compound of Formula 1, the use of said process in the preparation of a compound of Formula 5 or a phosphate, sulphate, hydrogensulphate, malate, citrate, tartrate or fumarate salt thereof, and the use of the fumarate salt in a composition for use in therapy.Type: ApplicationFiled: June 18, 2009Publication date: December 24, 2009Applicant: AstraZeneca ABInventors: Helen Blade, Gwydion Huw Churchill, Angela Charlotte Currie, Benjamin Charles Dobson, Martin Neal Kenworthy, Lyn Powell, Steven Anthony Raw, Peter Samuel Hynes
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Patent number: 7622497Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 17, 2004Date of Patent: November 24, 2009Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
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Publication number: 20090258857Abstract: The present invention encompasses compounds of general formula (1) wherein R1, M1, L1 and Q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell proliferation, and the use thereof for preparing a pharmaceutical composition with the above-mentioned properties.Type: ApplicationFiled: June 13, 2007Publication date: October 15, 2009Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich Reiser, Peter Ettmayer, Oliver Kraemer, Peter Sennhenn, Walter Spevak
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Publication number: 20090253694Abstract: This invention provides fused heterocyclic compounds, pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12 related disease and disorders.Type: ApplicationFiled: February 20, 2009Publication date: October 8, 2009Applicant: Synta Pharmaceuticals Corp.Inventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Teresa Przewloka, Hao Li, Zachary Demko, Dinesh Chimmanamada
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Publication number: 20090247513Abstract: Benzothiophene compounds such as are DNA binding compounds exhibiting antibacterial activity.Type: ApplicationFiled: December 4, 2007Publication date: October 1, 2009Applicant: GeneSoft Pharmaceuticals, Inc.Inventors: Roland W. Burli, Eldon E. Baird, Matthew J. Taylor, Jacob A. Kaizerman, Wenhao Hu
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Publication number: 20090221568Abstract: FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2??-hydroxy-5?-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.Type: ApplicationFiled: November 3, 2006Publication date: September 3, 2009Inventors: Jared Shaw, Sameer Urgaonkar, Debabrata RayChaudhuri, Henry La Pierre
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Patent number: 7576079Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; ?represents either a single or a double bond; R2 is selected from 6 or 10-membered aryl and Het, each optionally substituted with R20; provided that Het is not a 5- or 6-membered monocyclic heterocycle having 1 or 2 nitrogen heteroatoms; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-arylType: GrantFiled: January 17, 2006Date of Patent: August 18, 2009Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, James Gillard, Marc-Andre Poupart
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Publication number: 20090181957Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthmaType: ApplicationFiled: March 2, 2006Publication date: July 16, 2009Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Publication number: 20090143368Abstract: A composition for inhibiting the extracellular matrix gene transcription comprising a cinnamoyl compound represented by the formula (I): and an inert carrier, or the like.Type: ApplicationFiled: March 2, 2006Publication date: June 4, 2009Inventors: Hiroaki Shiraki, Kiyoshi Higashi, Yoshitaka Tomigahara, Junya Takahashi
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Publication number: 20090137579Abstract: The present invention is directed to the compound of formula (II), or a solvate thereof, or crystalline forms thereof; to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula (II), including crystalline forms thereof, and a pharmaceutically acceptable carrier; and to the use of a compound of formula (II), or crystalline forms thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting IKK-2, and methods related thereto.Type: ApplicationFiled: October 22, 2008Publication date: May 28, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Frederick A. Hicks, Martin Ian Cooper, Marianne Langston, Adrian St. Clair Brown
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Publication number: 20090131422Abstract: The present invention is directed to the Tartrate, Mono-Hydrochloride, Malonate and p-Toluenesulfonate Salts of the compound of formula (I), or solvates thereof, or crystalline forms thereof; to a pharmaceutical composition comprising a pharmaceutically effective amount of the Salts, including crystalline forms thereof, and a pharmaceutically acceptable carrier; and to the use of the Salts, including crystalline forms thereof, for treating a patient suffering from, or subject to, a pathological condition capable of being ameliorated by inhibiting IKK-2, and methods related thereto.Type: ApplicationFiled: October 22, 2008Publication date: May 21, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Frederick A. Hicks, Martin Ian Cooper, Adrian St Clair Brown
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Publication number: 20090111803Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
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Publication number: 20090042865Abstract: A compound of formula I: wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; X is CH or N; n is 1 or 2; RC1 and RC2 are independently selected from H and methyl; when X is N, RX is selected from the group consisting of H, and optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, acyl, ester, amido and sulfonyl; and when X is CH, RX is selected from the group consisting of H, and optionally substituted C1-7 alkyl, C3-20 heterocyclyl, C5-20 aryl, acyl, ester, amido, sulfonyl, amino and ether.Type: ApplicationFiled: July 18, 2008Publication date: February 12, 2009Inventors: Mark Frigerio, Marc Geoffrey Hummersone, Keith Allan Menear, Christine Sarah Bailey, Heather Mary Ellen Duggan, Sylvie Gomez, Niall Morrison Barr Martin
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Publication number: 20090029955Abstract: A pyridothienopyrimidine derivative of formula (I), or the pharmaceutically acceptable salts or N-oxides thereof are disclosed, as well as pharmaceutical compositions comprising said compounds and methods of treatment or prevention of a pathological condition or disease susceptible to amelioration by inhibition of phosphodiesterase 4 using said compounds are disclosed.Type: ApplicationFiled: November 30, 2005Publication date: January 29, 2009Inventors: Lluis Miquel Pages Santacana, Joan Taltavull Moll
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Patent number: 7482342Abstract: Compound corresponding to general formula (I): in which, R1 represents a hydrogen or halogen atom, an NH2, NHR2, NHCOR2, NO2, CN, CH2NH2 and CH2NHR2; or alternatively R1 represents an optionally substituted phenyl or an optionally substituted heteroaromatic group; Ar represents an optionally substituted phenyl group or an optionally substituted heteroaromatic group; n represents 0, 1, 2 or 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Application in therapy.Type: GrantFiled: April 1, 2005Date of Patent: January 27, 2009Assignee: sanofi-aventisInventors: Hugues D'Orchymont, Luc Van Hijfte, Andre Zimmermann
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Publication number: 20090023719Abstract: A compound of formula (I) where one of A1, A2 or A3 is N, and the others are independently selected from CH or N; ring B is a fused 5 or 6-membered carbocyclic or heterocyclic which is optionally substituted as defined in the specification, and R1, R2, R3, R4, and n are as defined in the specification. The compounds are inhibitors of EphB4 or EphA2 and therefore may be useful in pharmaceutical compositions for the treatment of conditions such as cancer.Type: ApplicationFiled: July 16, 2008Publication date: January 22, 2009Applicant: Astrazeneca ABInventors: Bernard Christophe Barlaam, Richard Ducray, Jason Grant Kettle
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Publication number: 20080311076Abstract: Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses, wherein R1, R2, R3 and R4 are as defined in the claims.Type: ApplicationFiled: April 28, 2005Publication date: December 18, 2008Applicant: ARROW THERAPEUTICS LIMITEDInventors: Keith Charles Spencer, Helena Dennison, Neil Mathews, Michael Christopher Barnes, Surinder Singh Chana
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Publication number: 20080312223Abstract: The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or —(CH2)m—(B)n—; B is C?O, NR8(C?O) or O(C?O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; Ro is hydrogen or, together with NRg when present, forms a group —(CH2)p— wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyType: ApplicationFiled: December 30, 2005Publication date: December 18, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Michael Alistair O'Brien, Theresa Rachel Phillips, Paul Graham Wyatt
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080300244Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: December 13, 2007Publication date: December 4, 2008Applicant: AstraZeneca ABInventors: Roger Victor BONNERT, Thomas McInally, Tobias Mochel, Stephen Thom
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Publication number: 20080267914Abstract: Compounds of formula (Ia) are found to be active in inhibiting replication of flaviviridae viruses (Ia), wherein R1 and R2 are the same or different and represent hydrogen, halogen, -L-O—R3, -L-O-L-A or -L-O-L?-A?, wherein each L is the same or different and represents a direct bond or a C1-C4 alkylene group; L? represents a direct bond or a C2-C4 alkylene group; R3 represents hydrogen, C1-C4 alkyl or C1-C4 haloalkyl; A represents a 5- to 10-membered heterocyclyl group; and A? represents a C6-C1 aryl group; wherein at least one of R1 and R2 is -L-O—R3, -L-O-L-A or -L-O-L?-A?.Type: ApplicationFiled: October 9, 2006Publication date: October 30, 2008Inventors: Michael Christopher Barnes, Surinder Singh Chana, Helena Dennison, Lyn Jennens, Neil Mathews, Christopher John Pilkington, Keith Charles Spencer, Alexander James Floyd Thomas
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Publication number: 20080221096Abstract: The present disclosure relates to a pyridofuropyrimidine derivative of formula (I): wherein G1 is a group chosen from —CR6R7— and —O— wherein R6 and R7 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R1 and R2 are independently chosen from hydrogen atoms and C1-4 alkyl groups; R3 is chosen from C1-4 alkyl, C1-4 alkoxy, amino, hydroxy, mono-C1-4alkylamino, di-C1-4alkylamino, C3-8cycloalkylamino, aryl, heteroaryl and saturated N-containing heterocyclyl groups which are bound to the pyridine ring through their nitrogen atom, all of them being optionally substituted by one or more substituents chosen from halogen atoms and hydroxy, C1-4 alkyl, C1-4alkoxy-C1-4alkyl, aryl-C1-4alkyl, —O(CO)OR8, C1-4 alkoxy, —(CO)NR8R9, —CN, —CF3, —NR8R9, —SR8 and —SO2NH2 groups wherein R8 and R9 are each independently chosen from a hydrogen atom or a C1-4 alkyl group; R4 and R5 are independently chosen from hydrogen atoms, C1-4alkyl groups, hydroxyl-C1-4alkyl groups and groups of formula (II): wherein p aType: ApplicationFiled: July 21, 2006Publication date: September 11, 2008Inventors: Joan Taltavull Moll, Luis Miguel Pages Santacana
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Publication number: 20080207609Abstract: Fused pyrimidines of formula (I): wherein R1-R3, A and n have any of the values described in the specification; and pharmaceutically acceptable salts thereof; have activity as inhibitors of PI3K and may thus be used to treat diseases and disorders arising from abnormal cell growth, function or behavior associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.Type: ApplicationFiled: August 16, 2007Publication date: August 28, 2008Applicant: Plramed LimitedInventors: Stephen J. Shuttleworth, Adrian J. Folkes, Irina S. Chuckowree, Nan Chi Wan, Timothy C. Hancox, Stewart J. Baker, Sukhjit Sohal, Mohammed A. Latif
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Patent number: 7417066Abstract: The invention relates to compounds of general Formula I, the production thereof, and the use thereof as a medicinal product.Type: GrantFiled: June 7, 2006Date of Patent: August 26, 2008Assignee: Schering AGInventors: Bernd Buchmann, Martin Fritsch, Duy Nguyen, Bernd Menzenbach, Ulf Boemer
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Patent number: 7414073Abstract: Included within the scope of the present invention are potent taxanes and taxanes containing a linking group. Also included is a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for inducing cell death in selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a link, and (B) a pharmaceutically acceptable carrier, diluent or excipient is also included. A method for inducing cell death in selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent is included as well.Type: GrantFiled: October 14, 2004Date of Patent: August 19, 2008Assignee: Immunogen Inc.Inventors: Erkan Baloglu, Michael Miller, Ravi V. J. Chari
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Publication number: 20080194546Abstract: There is provided a compound of formula I: wherein: one or two of X5, X6 and X8 is N, and the others are CH; R7 is selected from halo, ORO1, SRS1, NRN1RN2, NRN7aC(?O)RC1, NRN7bSO2RS2a, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C5-20 aryl group, where RO1 and RS1 are selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, or an optionally substituted C1-7 alkyl group; RN1 and RN2 are independently selected from H, an optionally substituted C1-7 alkyl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C5-20 aryl group or RN1 and RN2 together with the nitrogen to which they are bound form a heterocyclic ring containing between 3 and 8 ring atoms; RC1 is selected from H, an optionally substituted C5-20 aryl group, an optionally substituted C5-20 heteroaryl group, an optionally substituted C1-7 alkyl group or NRN8RN9, where RN8 and RN9 are independently selected from H, an optionally subsType: ApplicationFiled: August 21, 2007Publication date: August 14, 2008Applicant: KuDOS Pharmaceuticals LimitedInventors: Marc Geoffrey Hummersone, Gomez Sylvie, Keith Allan Menear, Graeme Cameron Murray Smith, Karine Malagu, Heather Mary Ellen Duggan, Niall Morrison Barr Martin, Frederic Georges Marie Leroux, Gesine Johanna Hermann, Xiao-Ling Fan Cockcroft
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Patent number: 7410990Abstract: This invention features a compound of formula (I): R1 is aryl or heteroaryl; each of R2 and R4, independently, is H, halogen, CN, alkyl, ORa, or NRaRb; R3 is H, halogen, CN, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, heterocyclyl, ORa, OC(O)Ra, OC(O)NRaRb, NRaRb, NRaC(O)Rb, NRaS(O)RbNRaS(O)2Rb, NRaC(O)NRbRc, NRaC(S)NRbRc, NRaC(NRb)NRcRd, NRaC(O)ORb, S(O)NRaRb, S(O)2NRaRb, S(O)Ra, S(O)2Ra, C(O)Ra, C(O)ORa, or C(O)NRaRb; R5 is H or alkyl; n is 0, 1, 2, 3, 4, 5, or 6; A is O, S, S(O), S(O)2, or NRe; B is N or CRf; X is O, S, S(O), S(O)2, NRe, or C(O); Y is a covalent bond, C(O), C?NRa, O, S, S(O), S(O)2, or NRe; Z is N or CH; each of U and V, independently, is N or CR; and W is O, S, or NRe; in which each of Ra, Rb, Rc, and Rd, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; Re is H, alkyl, aryl, acyl, or sufonyl; and Rf is H, alkyl, aryl, acyl, sulfonyl, alkoxyl, amino, ester, amide, CN, or halogen.Type: GrantFiled: October 3, 2006Date of Patent: August 12, 2008Assignee: Synta Pharmaceuticals Corp.Inventors: Lijun Sun, Mitsunori Ono, Yumiko Wada, Weiwen Ying, Teresa Przewloka, Elena Kostik
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Patent number: 7405211Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.Type: GrantFiled: October 12, 2004Date of Patent: July 29, 2008Assignee: AstraZeneca ABInventors: Alan D. Robertson, Shaun Jackson, Vijaya Kenche, Cindy Yaip, Hishani Parbaharan, Phil Thompson
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Patent number: 7396828Abstract: The invention provides prodrugs of inhibitors of PI-3 kinase. The compounds are LY294002 and analogs thereof comprising a reversibly quaternized amine.Type: GrantFiled: April 20, 2005Date of Patent: July 8, 2008Assignee: Semafore Pharmaceuticals, Inc.Inventors: Joseph R. Garlich, Donald L. Durden, Mary Patterson, Jingdong Su, Robert G. Suhr
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Publication number: 20080146555Abstract: The invention pertains to inhibitors of various kinases (e.g. S/T kinases, Tyr kinases, etc.), which inhibitors are previously known as cyclin dependent kinase inhibitors (CDKs). As described herein, the inhibitors of this invention are capable of inhibiting various wild-type and mutant form kinases, including drug resistant forms of mutant kinases. Thus the subject kinase inhibitors are useful in treating a wide range of diseases/conditions associated with abnormal functions/excessive activities of the target kinases, including mutant kinases. The invention further provides methods for treating cancers, tumors and patients which are resistant or refractory to other therapeutic agents. Pharmaceutical compositions and packaged pharmaceuticals with instructions of these inhibitors, and methods of using these inhibitors are also provided.Type: ApplicationFiled: June 17, 2005Publication date: June 19, 2008Applicant: GPC Biotech, IncInventors: Maureen G. Caligiuri, Nikolai A. Kley, Krishna K. Murthi
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Patent number: 7378421Abstract: Novel compounds of the formula I in which R1, R2, R3 and Het are as defined herein, which are inhibitors of tyrosine kinases and/or Raf kinases and can be employed for the treatment of tumours, for neuroprotection and for protection of the stress proteins of the skin.Type: GrantFiled: April 28, 2004Date of Patent: May 27, 2008Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Teresa Mujica-Fernaud, Herwig Buchholz, Wilfried Rautenberg, Christian Sirrenberg
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Patent number: 7358247Abstract: Provided is an impurity of mycophenolate mofetil, processes for its preparation and its use as a reference.Type: GrantFiled: April 26, 2005Date of Patent: April 15, 2008Assignee: TEVA Gyógyszergyár Zártköruen Muködö RészvénytársaságInventors: Sandor Molnar, Tivadar Tamas, Janos Hajko, Beáta Kosztya, Amihai Eisenstadt
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Publication number: 20080064679Abstract: Water-soluble cannabinoid compounds that are agonists of CB1 and CB2 cannabinoid receptors are provided. The compounds are made water-soluble by derivatization of the alkyl side chain and/or the phenolic hydroxyl group of tetrahydrocannabinol. The water-soluble cannabinoids are useful for the treatment of appetite loss, pain, multiple sclerosis, nausea and vomiting, and epilepsy.Type: ApplicationFiled: June 23, 2005Publication date: March 13, 2008Inventors: Billy R. Martin, Raj K. Razdan, Anu Mahadevan
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Patent number: 7300930Abstract: The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is ?O, L is —H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula —N(RN)Q, wherein: RN is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptablType: GrantFiled: June 22, 2005Date of Patent: November 27, 2007Assignee: Cancer Research Technology LimitedInventors: Stephen Neidle, Richard John Harrison, Lloyd Royston Kelland, Sharon Michele Gowan, Martin Anthony Read, Anthony Reszka
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Patent number: 7268143Abstract: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.Type: GrantFiled: October 12, 2004Date of Patent: September 11, 2007Assignee: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo, Andrew L. Salzman, Aloka Roy, William Williams
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Patent number: 7265103Abstract: The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on the phenylpart of the tricyclic moiety with primary, secondary and/or tertiary amino groups, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2 and R3 are certain specific substituents, with the proviso that at least one of R1 and R2 is an amino radical of formula N—R10R11 wherein R10 and R11 are each a variety of radicals, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutiType: GrantFiled: March 27, 2003Date of Patent: September 4, 2007Assignee: Janssen Pharmaceutica NV.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Margaretha Henrica Maria Bakker, Ana Isabel De Lucas Olivares
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Patent number: 7253284Abstract: Compounds of the formula I, Wherein X is N, n is 1 and R2and R3 together form a ring, R, R1 and R4 are as defined in the specifications.Type: GrantFiled: July 15, 2002Date of Patent: August 7, 2007Assignee: Giaxo Group LimitedInventors: Romano Di Fabio, Fabrizio Micheli, Yves St-Denis
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Patent number: 7253165Abstract: The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: May 12, 2004Date of Patent: August 7, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Gregory M. Shutske, James A. Hendrix, John G. Jurcak, Brian S. Freed, Nicholas J. Hrib, John D. Tomer, IV, Reda G. Hanna